Diversity-Oriented Synthesis of Imidazo-Dipyridines with Anticancer Activity via the Groebke–Blackburn–Bienaymé and TBAB-Mediated Cascade Reaction in One Pot

2019 ◽  
Vol 84 (19) ◽  
pp. 12632-12638 ◽  
Author(s):  
Yong Li ◽  
Jiu-Hong Huang ◽  
Juan-Li Wang ◽  
Gui-Ting Song ◽  
Dian-Yong Tang ◽  
...  
2018 ◽  
Vol 360 (19) ◽  
pp. 3655-3661 ◽  
Author(s):  
Gui-Ting Song ◽  
Nicholas McConnell ◽  
Zhong-Zhu Chen ◽  
Xiao-Fang Yao ◽  
Jiu-Hong Huang ◽  
...  

2018 ◽  
Vol 16 (33) ◽  
pp. 6096-6105 ◽  
Author(s):  
Xing Gao ◽  
Chunhui Shan ◽  
Zhihao Chen ◽  
Yan Liu ◽  
Xia Zhao ◽  
...  

A diversity-oriented synthesis of β-lactams via Ugi/Michael reaction cascades under mild conditions was achieved.


2018 ◽  
Vol 24 (26) ◽  
pp. 6732-6736 ◽  
Author(s):  
Zhi-Gang Xu ◽  
Shi-Qiang Li ◽  
Jiang-Ping Meng ◽  
Dian-Yong Tang ◽  
Liu-Jun He ◽  
...  

Author(s):  
Rajesh P. ◽  
Abdulrahman I. Almansour ◽  
Natarajan Arumugam ◽  
Srinivasarao Yaragorla

We report a one-pot, three-component, solvent-free, cascade reaction for the synthesis of 3-aminofurans using a calcium catalyst, in which, the in situ formed C,N-diacyliminium ion, is the key intermediate.


2020 ◽  
Vol 17 (10) ◽  
pp. 772-778
Author(s):  
Abdulrhman Alsayari ◽  
Abdullatif Bin Muhsinah ◽  
Yahya I. Asiri ◽  
Jaber Abdullah Alshehri ◽  
Yahia N. Mabkhot ◽  
...  

The aim of this study was to synthesize and evaluate the biological activity of pyrazole derivatives, in particular, to perform a “greener” one-pot synthesis using a solvent-free method as an alternative strategy for synthesizing hydrazono/diazenyl-pyridine-pyrazole hybrid molecules with potential anticancer activity. Effective treatment for all types of cancers is still a long way in the future due to the severe adverse drug reactions and drug resistance associated with current drugs. Therefore, there is a pressing need to develop safer and more effective anticancer agents. In this context, some hybrid analogues containing the bioactive pharmacophores viz. pyrazole, pyridine, and diazo scaffolds were synthesized by one-pot method. Herein, we describe the expedient synthesis of pyrazoles by a onepot three-component condensation of ethyl acetoacetate/acetylacetone, isoniazid, and arenediazonium salts under solvent-free conditions, and the evaluation of their cytotoxicity using a sulforhodamine B assay on three cancer cell lines. Molecular docking studies employing tyrosine kinase were also carried out to evaluate the binding mode of the pyrazole derivatives under study. 1-(4-Pyridinylcarbonyl)-3- methyl-4-(2-arylhydrazono)-2-pyrazolin-5-ones and [4-(2-aryldiazenyl)-3,5-dimethyl-1H-pyrazol-1- yl]-4-pyridinylmethanones, previously described, were prepared using an improved procedure. Among these ten products, 1-isonicotinoyl-3-methyl-4-[2-(4-nitrophenyl)hydrazono]-2-pyrazolin-5-one (1f) displayed promising anticancer activity against the MCF-7, HepG2 and HCT-116 cell lines, with an IC50 value in the range of 0.2-3.4 μM. In summary, our findings suggest that pyrazoles containing hydrazono/ diazenyl and pyridine pharmacophores constitute promising scaffolds for the development of new anticancer agents.


Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 1131
Author(s):  
Perumal Gobinath ◽  
Ponnusamy Packialakshmi ◽  
Ali Daoud ◽  
Saud Alarifi ◽  
Akbar Idhayadhulla ◽  
...  

In the original article [...]


2021 ◽  
Vol 6 (29) ◽  
pp. 7306-7316
Author(s):  
Marwa Abdel‐Motaal ◽  
Fardous F. El‐Senduny ◽  
Saad Shaaban

ChemInform ◽  
2014 ◽  
Vol 45 (24) ◽  
pp. no-no
Author(s):  
Shuyan Zheng ◽  
Hongsheng Tan ◽  
Xiaoguang Zhang ◽  
Chunhui Yu ◽  
Zhengwu Shen
Keyword(s):  

2013 ◽  
Vol 54 (6) ◽  
pp. 506-511 ◽  
Author(s):  
Hiromi Uchiro ◽  
Nobuhiro Shionozaki ◽  
Ryo Tanaka ◽  
Hiroyuki Kitano ◽  
Naoki Iwamura ◽  
...  

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